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BRPI0804121A2 - methods for the resolution of 4- [4- (dimethylamino) -1- (4'-fluoro-phenyl) -1-hydroxy-butyl] -3- (hydroxymethyl) -benzonitrile as a racemic or non-racemic mixture. of enanciomers in their isolated enanciomers and for the manufacture of escitalopram - Google Patents

methods for the resolution of 4- [4- (dimethylamino) -1- (4'-fluoro-phenyl) -1-hydroxy-butyl] -3- (hydroxymethyl) -benzonitrile as a racemic or non-racemic mixture. of enanciomers in their isolated enanciomers and for the manufacture of escitalopram

Info

Publication number
BRPI0804121A2
BRPI0804121A2 BRPI0804121-0A BRPI0804121A BRPI0804121A2 BR PI0804121 A2 BRPI0804121 A2 BR PI0804121A2 BR PI0804121 A BRPI0804121 A BR PI0804121A BR PI0804121 A2 BRPI0804121 A2 BR PI0804121A2
Authority
BR
Brazil
Prior art keywords
enanciomers
racemic
hydroxy
fluoro
phenyl
Prior art date
Application number
BRPI0804121-0A
Other languages
Portuguese (pt)
Inventor
Faveri Carla De
Florian Anton Martin Huber
Robert James Dancer
Original Assignee
Lundbeck & Co As H
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39735675&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0804121(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Lundbeck & Co As H filed Critical Lundbeck & Co As H
Publication of BRPI0804121A2 publication Critical patent/BRPI0804121A2/en
Publication of BRPI0804121A8 publication Critical patent/BRPI0804121A8/en
Publication of BRPI0804121B1 publication Critical patent/BRPI0804121B1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87Benzo [c] furans; Hydrogenated benzo [c] furans
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C253/00Preparation of carboxylic acid nitriles
    • C07C253/32Separation; Purification; Stabilisation; Use of additives
    • C07C253/34Separation; Purification
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/53Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and hydroxy groups bound to the carbon skeleton

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

MéTODOS PARA A RESOLUçãO DE 4-[4-(DIMETIL-AMINO)-1-(4'-FLUORO-FENIL)- 1 -HIDRóXI-BUTIL] -3 -(HIDRóXI-METIL)-BENZONITRILA COMO UMA MISTURA RACêMICA OU NãO-RACêMICA DE ENANCIÈMEROS EM SEUS ENANCIÈMEROS ISOLADOS E PARA A MANUFATURA DE ESCITALOPRAM. Esta patente descreve um método para a resolução de 4-[4-(dimetil-amino)- 1 -(4'-fluoro-fenil)- 1 -hidróxi-butil] -3 -(hidróxi-metil)-benzonitrila como uma mistura racêmica ou não-racêmica de enanciómeros em seus enanciómeros isolados, o citado método compreendendo as etapas de fracionadamente cristalizar 4-[4-(dimetil-amino)- 1 -(4'-fluoro-fenil)- 1 -hidróxi-butil]-3-(hidróxi-metil)-benzonitrila como um sal com o (+)-(S,S) ou (R,R)-enanciómero de ácido O, O'-di-p-toluoil-tartárico em um sistema de solvente compreendendo 1 -propanol, etanol ou acetonitrila.METHODS FOR SOLVING 4- [4- (DIMETHYL-AMINO) -1- (4'-FLUORO-PHENYL) - 1-HYDROXY-butyl] -3- (HYDROXY-METHYL) -BENZONITRIL AS A RACEMIC OR NOT RACEMIC OF ENANCIEMEROS IN ITS ISOLATED ENANCIEMERS AND FOR MANUFACTURE OF ESCITALOPRAM. This patent describes a method for the resolution of 4- [4- (dimethylamino) -1- (4'-fluoro-phenyl) -1-hydroxy-butyl] -3- (hydroxymethyl) -benzonitrile as a mixture racemic or non-racemic of enanciomers in their isolated enanciomers, said method comprising the steps of fractionally crystallizing 4- [4- (dimethylamino) -1- (4'-fluoro-phenyl) -1-hydroxy-butyl] - 3- (hydroxymethyl) benzonitrile as a salt with the O, O'-di-p-toluoyl tartaric acid (+) - (S, S) or (R, R) -enanciomer in a solvent system comprising 1-propanol, ethanol or acetonitrile.

BRPI0804121-0A 2007-09-11 2008-09-11 METHOD FOR THE RESOLUTION OF 4-[4-(DIMETHYL-AMINO)-1-(4'FLUORO-PHENYL)-1-HYDROXY-BUTYL]-3-(HYDROXY-METHYL)-BENZONITRILE AS A RACEMIC OR NON-RACEMIC MIXTURE OF ENANCIOMERS IN THEIR ISOLATED ENANCIOMERS BRPI0804121B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA200701314 2007-09-11
DKPA200701314 2007-09-11

Publications (3)

Publication Number Publication Date
BRPI0804121A2 true BRPI0804121A2 (en) 2009-09-29
BRPI0804121A8 BRPI0804121A8 (en) 2021-04-13
BRPI0804121B1 BRPI0804121B1 (en) 2022-04-12

Family

ID=39735675

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0804121-0A BRPI0804121B1 (en) 2007-09-11 2008-09-11 METHOD FOR THE RESOLUTION OF 4-[4-(DIMETHYL-AMINO)-1-(4'FLUORO-PHENYL)-1-HYDROXY-BUTYL]-3-(HYDROXY-METHYL)-BENZONITRILE AS A RACEMIC OR NON-RACEMIC MIXTURE OF ENANCIOMERS IN THEIR ISOLATED ENANCIOMERS

Country Status (52)

Country Link
EP (2) EP2061753B1 (en)
JP (1) JP4966933B2 (en)
KR (1) KR101054224B1 (en)
CN (1) CN101386583A (en)
AR (2) AR068174A1 (en)
AT (2) ATE518829T1 (en)
AU (1) AU2008212055C1 (en)
BE (1) BE1017548A6 (en)
BG (1) BG110206A (en)
BR (1) BRPI0804121B1 (en)
CA (1) CA2638499C (en)
CH (1) CH697885B1 (en)
CL (1) CL2008002686A1 (en)
CO (1) CO6140012A1 (en)
CY (2) CY2600B1 (en)
CZ (1) CZ2008537A3 (en)
DE (1) DE102008046530A1 (en)
DK (2) DK177075B1 (en)
EA (1) EA012787B1 (en)
EE (1) EE00864U1 (en)
ES (2) ES2368294T3 (en)
FI (1) FI121570B (en)
FR (1) FR2920766A1 (en)
GB (1) GB2448848B (en)
GR (1) GR1006595B (en)
HR (2) HRP20080425A2 (en)
HU (1) HUP0800549A2 (en)
IE (1) IES20080708A2 (en)
IL (1) IL193845A (en)
IS (1) IS8758A (en)
LT (1) LT5577B (en)
LU (1) LU91479B1 (en)
LV (1) LV13813B (en)
ME (1) ME00176B (en)
MX (1) MX2008011451A (en)
MY (1) MY144210A (en)
NL (1) NL2001953C2 (en)
NO (1) NO20083756L (en)
NZ (1) NZ570884A (en)
PL (2) PL386026A1 (en)
PT (2) PT104169A (en)
RO (1) RO125301A2 (en)
RS (2) RS20080401A (en)
SE (1) SE533041C2 (en)
SG (1) SG151195A1 (en)
SI (2) SI22567A2 (en)
SK (1) SK500302008A3 (en)
TR (2) TR200907629A2 (en)
TW (1) TWI391383B (en)
UA (2) UA43461U (en)
WO (1) WO2009033488A1 (en)
ZA (1) ZA200807753B (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1987016A1 (en) 2005-07-27 2008-11-05 Aurobindo Pharma Limited An improved process for the preparation of escitalopram
CN102796065A (en) * 2011-05-27 2012-11-28 江苏豪森医药集团连云港宏创医药有限公司 Method for preparing high-optical-purity escitalopram
CN104119240A (en) * 2013-04-23 2014-10-29 中国人民解放军军事医学科学院毒物药物研究所 Preparation method for (S)-(-)-alpha-methylaminopropiophenone
CN103497145B (en) * 2013-10-10 2016-01-27 南昌大学 A kind of preparation technology of optical purity E2020
CN104119248A (en) * 2014-08-08 2014-10-29 广东东阳光药业有限公司 The preparation method of S-citalopram
CN107074750B (en) 2014-11-14 2022-03-25 浙江华海药业股份有限公司 A kind of method for splitting citalopram intermediate 5-cyanodiol

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8814057D0 (en) * 1988-06-14 1988-07-20 Lundbeck & Co As H New enantiomers & their isolation
AR034612A1 (en) 2001-06-25 2004-03-03 Lundbeck & Co As H PROCESS FOR THE PREPARATION OF RACEMIC CITALOPRAM AND / OR OF THE S- OR R-CITALOPRAM THROUGH THE SEPARATION OF A MIXING OF R- AND S-CITALOPRAM
AR034759A1 (en) * 2001-07-13 2004-03-17 Lundbeck & Co As H METHOD FOR THE PREPARATION OF ESCITALOPRAM
IS7239A (en) * 2001-12-14 2004-04-29 H. Lundbeck A/S Process for the production of acitalopram
CA2511143C (en) 2002-12-23 2011-06-28 H. Lundbeck A/S Preparation of racemic and/or s- or r-citalopram diols and their use for the preparation racemic and/or s- or r-citalopram
AU2003242990A1 (en) * 2003-01-17 2004-08-13 Pulla Reddy Muddasani Processes for the preparation of escitalopram and its precursor
WO2005047274A1 (en) * 2003-11-12 2005-05-26 Dr. Reddy's Laboratories, Inc. Preparation of escitalopram
EP1877394A1 (en) * 2005-04-04 2008-01-16 Jubilant Organosys Limited Process for the preparation of escitalopram or its acid addition salts
EP1987016A1 (en) * 2005-07-27 2008-11-05 Aurobindo Pharma Limited An improved process for the preparation of escitalopram

Also Published As

Publication number Publication date
HUP0800549A2 (en) 2009-03-02
HU0800549D0 (en) 2008-10-28
FI20085807A0 (en) 2008-08-29
SE0801929L (en) 2009-03-12
NZ570884A (en) 2010-03-26
TWI391383B (en) 2013-04-01
TW200906814A (en) 2009-02-16
CZ2008537A3 (en) 2009-03-18
ES2334875A1 (en) 2010-03-16
EE00864U1 (en) 2009-10-15
IL193845A (en) 2011-03-31
CO6140012A1 (en) 2010-03-19
AT10984U1 (en) 2010-02-15
FI121570B (en) 2011-01-14
MY144210A (en) 2011-08-15
AU2008212055B2 (en) 2010-08-12
IS8758A (en) 2009-03-12
EP2397461A1 (en) 2011-12-21
LT5577B (en) 2009-06-25
ZA200807753B (en) 2009-04-29
GR1006595B (en) 2009-11-16
PT2061753E (en) 2011-09-14
EP2061753B1 (en) 2011-08-03
SK500302008A3 (en) 2009-04-06
FR2920766A1 (en) 2009-03-13
PL2061753T3 (en) 2011-12-30
BG110206A (en) 2009-03-31
JP4966933B2 (en) 2012-07-04
SG151195A1 (en) 2009-04-30
SE533041C2 (en) 2010-06-15
AR108885A2 (en) 2018-10-03
MEP10108A (en) 2010-10-10
UA41919U (en) 2009-06-10
CH697885B1 (en) 2009-03-13
CN101386583A (en) 2009-03-18
AU2008212055A1 (en) 2009-03-26
AU2008212055C1 (en) 2011-06-02
CA2638499C (en) 2010-09-28
RS51909B (en) 2012-02-29
CA2638499A1 (en) 2008-11-21
RO125301A2 (en) 2010-03-30
SI22567A2 (en) 2008-12-31
KR20090027185A (en) 2009-03-16
NO20083756L (en) 2009-03-12
ES2368294T3 (en) 2011-11-16
PT104169A (en) 2009-02-02
DK2061753T3 (en) 2011-09-26
LU91479B1 (en) 2010-03-11
TR200907629A2 (en) 2009-11-23
ME00176B (en) 2011-02-10
WO2009033488A1 (en) 2009-03-19
BE1017548A6 (en) 2008-11-04
PL386026A1 (en) 2009-02-16
UA43461U (en) 2009-08-25
MX2008011451A (en) 2009-03-10
EA200801797A2 (en) 2008-12-30
HRP20080425A2 (en) 2010-04-30
EA012787B1 (en) 2009-12-30
GB2448848A (en) 2008-10-29
RS20080401A (en) 2010-03-02
LT2008068A (en) 2009-03-25
CL2008002686A1 (en) 2009-01-02
LV13813B (en) 2008-11-20
IES20080708A2 (en) 2009-03-18
TR200806903A2 (en) 2009-03-23
GB2448848B (en) 2011-01-26
DK200801265A (en) 2009-03-12
EA200801797A3 (en) 2009-02-27
ES2334875B1 (en) 2010-10-27
NL2001953C2 (en) 2009-05-07
JP2009149600A (en) 2009-07-09
EP2061753A1 (en) 2009-05-27
NL2001953A1 (en) 2008-12-22
DK177075B1 (en) 2011-06-14
GR20080100581A (en) 2009-04-30
SI2061753T1 (en) 2011-10-28
CY2600B1 (en) 2010-03-03
ATE518829T1 (en) 2011-08-15
DE102008046530A1 (en) 2009-03-19
FI20085807L (en) 2009-03-12
BRPI0804121B1 (en) 2022-04-12
KR101054224B1 (en) 2011-08-08
AR068174A1 (en) 2009-11-11
HRP20110636T1 (en) 2011-10-31
CY1111924T1 (en) 2015-11-04
BRPI0804121A8 (en) 2021-04-13
GB0815773D0 (en) 2008-10-08

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